1477-44-7Relevant articles and documents
Structure-based design of glycyrrhetinic acid derivatives as potent anti-sepsis agents targeting high-mobility group box-1
Wang, Yuanyuan,Yu, Zongmin,Yuan, Hu,Chen, Hao,Xie, Ning,Wang, Zhibin,Sun, Qingyan,Zhang, Weidong
, (2020/11/27)
Novel Glycyrrhetinic Acid (GA) derivatives with fused heterocycles on A ring were structure-based designed and synthesized. Their potential anti-inflammatory effects were investigated by a classical LPS stimulated macrophage model. Surface plasmon resonance (SPR) was used to verify the binding of GA analogues with HMGB1. A preliminary structure–activity relationship was summarized and an analogue GA-60 with ortho-methoxybenzyl pyrozole showed stronger anti-inflammatory effect and higher affinity for HMGB1 with a Kd value of 12.5 μM. In addition, this compound exhibited excellent inhibitory functions on NO (96%), TNF-α (94%), and IL-6 (100%), by interfering with phosphorylation of p38, ERK, JNK MAPKs, as well as that of NF-κB p65 and IKKα/β. Moreover, GA-60 extended the survival of either the classic CLP-induced or LPS-induced sepsis mouse models. Molecular modeling predictions further supported these findings, clearly indicating that inhibiting HMGB1 release, using fused heterocyclic GA derivatives, is a promising strategy for treatment of sepsis.
Preparation method of 18 beta-methyl glycyrrhetinate
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Paragraph 0024; 0030-0063, (2021/11/27)
The invention provides a preparation method of 18 beta-methyl glycyrrhetinate, which comprises the following steps: taking 18 beta-glycyrrhetinic acid and trimethylsilyl diazomethane as raw materials, and reacting to prepare the 18 beta-methyl glycyrrhetinate. According to the invention, 18 beta-glycyrrhetinic acid is used as a starting material and is subjected to one-step methyl esterification reaction with trimethylsilyl diazomethane to obtain 18 beta-methyl glycyrrhetinate, the synthesis process is simple, the synthesis process conditions are mild, the yield is up to 99.2% or above, the product quality is good, and the content is greater than 99.5%. Besides, through selection of a plurality of parameters such as the solvent, the reaction time and the material dosage, the yield and the purity of the reaction are further improved, and a basis is provided for industrial production.
Quaternary ammonium glycyrrhetinic acid cationic surfactant as well as preparation method and application thereof (by machine translation)
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Paragraph 0041; 0043; 0044, (2020/05/01)
The invention discloses a quaternary ammonium glycyrrhetinic acid cationic surfactant and a preparation method and application. thereof, and the critical micelle concentration of the surfactant at room temperature is 5 × 10. - 4 mol/L, Can descend the surface tension from 72mN/m to 47mN/m. and, the surfactant has better regulation and control effect on the bouncing behavior of the liquid drop on the hydrophobic solid surface, and the surfactant concentration on the surface of the blade such as dive, PTFE can be 5 × 10 higher. - 4 At mol/L, can obviously inhibit the liquid drop bouncing, and realize better spreading. and, the quaternary ammonium glycyrrhetinic acid cationic surfactant in the invention can extend to various crop blades, such as wheat, rice, corn, cabbage and other blades, have great application prospects, in the field of agricultural industry. (by machine translation)
